G
Gary H. Rasmusson
Researcher at Merck & Co.
Publications - 154
Citations - 3731
Gary H. Rasmusson is an academic researcher from Merck & Co.. The author has contributed to research in topics: Alkyl & Reductase. The author has an hindex of 32, co-authored 154 publications receiving 3711 citations.
Papers
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Journal ArticleDOI
Azasteroids: structure-activity relationships for inhibition of 5.alpha.-reductase and of androgen receptor binding
Gary H. Rasmusson,Glenn F. Reynolds,Nathan G. Steinberg,Edward Walton,Gool F. Patel,Tehming Liang,Margaret A. Cascieri,Anne H. Cheung,J. R. Brooks,Charles Berman +9 more
TL;DR: A series of steroids were prepared and tested in vitro as inhibitors of human and rat prostatic 5 alpha-reductase and of binding of dihydrotestosterone to the rat androgen receptor and the primary structural modifications were changes of the A ring and of moieties attached at the C-17 position of the steroid nucleus.
Journal ArticleDOI
Azasteroids as inhibitors of rat prostatic 5 alpha-reductase.
Gary H. Rasmusson,Glenn F. Reynolds,Torleif Utne,Ronald B. Jobson,R. L. Primka,Charles Berman,J. R. Brooks +6 more
TL;DR: A series of A-ring heterocyclic steroids has been prepared and tested for inhibition of rat prostatic steroid 5 alpha-reductase in vitro and strikingly high inhibitory activity was found with a group of 17 beta-substituted 4-methyl-4-aza-5 alpha-androstan-3-ones.
Journal ArticleDOI
Species differences in prostatic steroid 5 alpha-reductases of rat, dog, and human.
TL;DR: The conversion of testosterone to 5a-dihydrotestosterone by prostate particulates from rats, dogs, and humans was investigated, and significant species differences were found with their pH profiles, affinities for 4-azasteroidal inhibitors, and sensitivities to mercuric sulfhydryl reagents.
Journal ArticleDOI
Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride: Enzyme-Catalyzed Formation of NADP−Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor
Herbert G. Bull,Margarita Garcia-Calvo,Stefan Andersson,Walter F. Baginsky,H. Karen Chan,Dina E. Ellsworth,Randall R. Miller,Ralph A. Stearns,Raman K. Bakshi,Gary H. Rasmusson,Richard L. Tolman,Robert W. Myers,and John W. Kozarich,Georgianna Harris +13 more
TL;DR: The intermediate NADP−dihydrofinasteride adduct can be recovered intact by denaturation of the enzyme−inhibitor complex and has been purified.
Patent
4-Aza-17 beta -substituted-5 alpha -androstan-3-one-reductase inhibitors
TL;DR: The A-homo analogs of the A-1.4-Aza-17 beta -substituted-5 alpha -androstan-3-ones and their A-Homo analog are active as testosterone 5 alpha -reductase inhibitors, and thus useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.